ライフサイエンスコーパス: druggable

1 hibition requires that the target protein be druggable.

2 cals suggesting Arc's synaptic action may be druggable.

3 roviding the proof of concept that EndoMT is druggable.

4 thways that were hitherto regarded as poorly druggable.

5 protein interaction site of MtTrxR is indeed druggable.

6 defined targets that are both essential and druggable.

7 also have associated proteins, which may be druggable.

8 A transient but druggable allosteric pocket in CDK2 is predicted to occu

9 PML nuclear bodies are druggable and could be harnessed in other conditions.

10 monstrates that HECT domains are potentially druggable and provides molecules that may be of experime

11 we validate that M. tuberculosis SerB2 is a druggable and suitable target to pursue for further high

12 Many of them are not druggable and therefore it is necessary to identify targ

13 e emerging from basic studies as potentially druggable and will surely be investigated.

14 hus they represent attractive anti-parasitic druggable and/or vaccine target.

15 p53 function in HTLV-1-transformed cells is "druggable" and can be restored by treatment with 9AA.

16 perceptions of what targets are considered "druggable" and provide support for drug design in beyond

17 ult of UppS inhibition, validating UppS as a druggable antibacterial target.

18 rate that FtsH1 is a novel and, importantly, druggable antimalarial target.

19 rus-host interactome identified 110 putative druggable antiviral targets and prioritized several exis

20 factors with the end goal of discovering new druggable antiviral targets.

21 Furthermore, a druggable AP-1 inhibitory small molecule suppresses skin

22 Identification of novel, non-classical and druggable AR-target genes may provide new approaches to

23 developed for the identification of the most druggable binding hot spots of proteins.

24 toward the prediction of hot spot regions in druggable binding pockets is illustrated by three test s

25 pied by these residues defines a potentially druggable binding site on NEMO that extends for ~16 A to

26 nd interactions is important for identifying druggable binding sites and for understanding how protei

27 imentally solved conformational ensembles of druggable binding sites in proteins, grouped by location

28 ed drug design consists in the prediction of druggable binding sites.

29 pproaches are required to reveal potentially druggable binding sites.

30 are critical for initiating food intake, but druggable biochemical pathways that control this respons

31 COMT is a druggable biological target for the treatment of various

32 trast to BET bromodomains, which have proven druggable, bromodomains from other regions of the phylog

33 cate the presence of several new potentially druggable BTK states.

34 and identify an anti-tumour target rendered druggable by cereblon modulation.

35 triggered by low [TF]wall, thrombosis may be druggable by contact pathway inhibition, although thromb

36 he method identifies targets that, while not druggable by druglike compounds, may become druggable us

37 teraction surfaces may not be intrinsically "druggable" by small molecules, and elevates in importanc

38 ding mode and allows the identification of a druggable cadherin interface, thus paving the way to a f

39 Kinase inhibitors feature strongly in the druggable cancer genome and 19 have been approved in onc

40 reens and a small-molecule screen focused on druggable cancer targets.

41 In addition, we uncovered a number of new druggable candidates because of their genomic alteration

42 Our approaches also uncovered many druggable candidates, and XPO1 was further explored as a

43 is dispensable for murine viability and has druggable catalytic activity.

44 Furthermore, relatives within druggable CATH functional families occupy central positi

45 milies that are currently enriched in drugs (druggable CATH functional families) and we use the netwo

46 Analysis of selected druggable CATH functional families, enriched in drug tar

47 he mutant Y220C that has a mutation-induced, druggable cavity.

48 e conducted an RNAi-based screen to identify druggable chromatin regulator-based targets in leukemias

49 iple genotypes of HCV and represents a novel druggable class of therapeutic targets for HCV infection

50 eplicon cell line (Luc-1b) with a kinome and druggable collection of 20,779 siRNAs.

51 thus, our analysis identifies a potentially "druggable" component of mtp53's gain-of-function activit

52 e a simple approach to distinguish them from druggable cryptic pockets.

53 identification of 69 proteins with potential druggable cryptic pockets.

54 potential; however, discerning critical and "druggable" effectors on a large scale will also require

55 he KRAS oncoprotein is, as yet, not directly druggable, efforts to target KRAS mutant cancers focus o

56 y are essential in breast cancer cell lines, druggable, enriched in stem-like breast cancer cells, an

57 ral progeny and thus provides an attractive, druggable enzymatic target.

58 irmed our previous finding that CYP27A1 is a druggable enzyme and found additional drugs as well as t

59 noma and are under regulation of potentially druggable enzymes.

60 that not all oncogenic driver proteins are "druggable" enzymes or receptors with activities that can

61 and progression, suggesting that apelin is a druggable factor in glioblastoma.

62 The total number of druggable gene claims has also increased by 30%.

63 nbiased discovery of potentially driving and druggable gene fusions in primary tumors.

64 siRNA)-based screening of approximately 4800 druggable genes in 3-dimensional CSLC cultures in compar

65 We identify 123 Bonferroni-significant druggable genes outside the MHC, and 128 FDR-significant

66 Our gene prediction approach prioritized druggable genes that are likely to be associated with Cr

67 xpression (MYC-SL) in a collection of ~3,300 druggable genes, using high-throughput siRNA screening.

68 m of drug-gene interactions and potentially 'druggable' genes.

69 gically normal controls, to find potentially druggable genetic targets.

70 The Illuminating the Druggable Genome (IDG) program was initiated in 2014, ha

71 screened a siRNA library against the entire druggable genome and a small-molecule library consisting

72 ionship network now defines a data-supported druggable genome encompassing 7% of human proteins.

73 ensive and user friendly tool for mining the druggable genome for precision medicine hypothesis gener

74 The 'druggable genome' encompasses several protein families,

75 coupled receptors, form a large part of the "druggable" genome.

76 enome-wide screening in the search for novel druggable host targets for adjunctive TB therapies.

77 oSite increases the size of the potentially "druggable" human proteome from ~40% to ~78% of disease-a

78 ting that many of the secondary sites may be druggable in nature with small molecules that could prov

79 a unique therapeutic approach to render Myc druggable in the clinic.

80 ated PPIs, uncovering a trove of potentially druggable interactions.

81 bitory effects in the nanomolar range toward druggable isoforms (hCA VII, hCA IX, and hCA XIV) (K(i)

82 r idea was to improve the selectivity toward druggable isoforms through the introduction of additiona

83 Together, our data reveal a druggable K2P site that stabilizes the C-type gate 'leak

84 Potentially druggable kinase fusions involving ALK, ROS, RET, NTRK a

85 ize a robust signaling network consisting of druggable kinase pathways.

86 We further identified 7 "druggable" kinases overexpressed across species.

87 Donecopride, as a druggable lead, was assessed for its in vivo procognitiv

88 and organoids and show that it depends on a druggable lipid-peroxidase pathway that protects against

89 novel molecular probes to further elucidate druggable mechanisms to improve cancer therapeutic respo

90 ve (normal) hosts and identifies potentially druggable microbial factors, such as pyruvate dehydrogen

91 inus of PrP(C) as a new and potentially more druggable molecular target for treating Alzheimer's dise

92 sequences, compounds, screening assays, and druggable molecular targets are being used by the worldw

93 n a variety of tumor models and represents a druggable molecular vulnerability with potential therape

94 AC) offers an optimal model for discovering "druggable" molecular pathways that participate in inflam

95 to prognostically relevant and potentially 'druggable' molecular targets are reviewed.

96 n data to pinpoint regulated subnetworks and druggable molecules.

97 we find that a consensus topology of highly druggable motifs consists of a negative feedback loop wi

98 Given the paucity of druggable mutations in high-risk neuroblastoma (NB), we

99 igorous criteria for defining and validating druggable mutations will be essential for the success of

100 predicted over 800 promising candidates for druggable mutations, raising new possibilities for desig

101 ndings of previously missed, but potentially druggable, mutations in the EGFR, MET and KIT oncogenes.

102 n mechanism of carcinogenesis and, given the druggable nature of these enzymes, an attractive target

103 ETD8, the H4(K20me1) methyltransferase, as a druggable NB target.

104 domain predictive algorithm for identifying druggable neighborhoods based on network parameters.

105 To discover druggable neuroprotective compounds for dopamine neurons

106 Thus, NAB identifies a druggable node in the biology of alpha-syn that can corr

107 ase 1 and 2 have been shown to be redundant, druggable nodes in the Wnt pathway.

108 ging, largely due to the relative paucity of druggable nodes in this pathway.

109 Much of the druggable non-olfactory human GPCR-ome remains under-int

110 We identified multiple potentially druggable, novel and known kinase fusions in diseases be

111 domain has been described as among the least druggable of that target class.

112 ocal amplifications, many of which contained druggable oncogenes (ERBB2, MET, FGFR1, CDK6, PIK3R3 and

113 fraction of tumors with aberrant activity of druggable oncoproteins despite a lack of mutations, and

114 in-5 has multiple allosteric sites that are "druggable." One site in particular, unique in its sequen

115 r suppressor gene mutations are not directly druggable, other proteins or pathways that become obliga

116 e net charge of a protein is not viewed as a druggable parameter.

117 tified oncostatin m signaling as a plausible druggable pathway for therapeutics.

118 lung cancers to GATA2 presents a network of druggable pathways for therapeutic exploitation.

119 ggest that GP130-dependent activation of the druggable PI3K/mTORC1 pathway is required for inflammati

120 This druggable pocket provides potentially complementary oppo

121 CCR2-RA-[R] binds in a novel, highly druggable pocket that is the most intracellular alloster

122 on with the AR AF-1 are within a potentially druggable pocket, implicating Bag-1L as a potential ther

123 Interrogation of a "druggable" pocket in the second zinc finger of KLF10 rev

124 mplex was screened for the presence of small druggable pockets formed from contributions from both pr

125 The high sequence conservation of druggable pockets of closely related proteins can make i

126 -p53 in the presence of DNA is revealed, and druggable pockets of p53 are identified via solvent mapp

127 In addition, the identification of druggable pockets or key intermediate conformations yiel

128 ein-protein interfaces, to indicate possible druggable pockets to be targeted by small molecules.

129 Because many proteins appear to lack druggable pockets, understanding and accurately identify

130 nd processive UTP incorporation, and predict druggable pockets.

131 kinase inhibition represents a potentially "druggable" point of intervention.

132 ve the potential to significantly expand the druggable portion of the proteome beyond traditional tar

133 out to investigate whether Galphai-GIV is a druggable PPI.

134 Targeting this druggable process could extend the lifespan of current f

135 tural platform to improve the efficiency and druggable properties of inhibitors.

136 cer; however, the contribution of conserved, druggable protein domains to this anticancer phenotype i

137 ) and we use the network properties of these druggable protein families to analyse their association

138 ining conformations is indeed a signature of druggable protein interaction sites and that analogous s

139 The miRNA screen led to identification of a druggable protein, ITGB1, whose functional inhibition sy

140 cesses raise hopes for routinely identifying druggable protein-protein interactions.

141 identified for >700 cysteines found in both druggable proteins and proteins deficient in chemical pr

142 t therapeutically, we searched for secreted, druggable proteins induced by Ras that are required for

143 cause of this problem, we sought to identify druggable proteins on the HCL surface that were dependen

144 Druggable proteins required for B lymphocyte survival an

145 Here, we use chemical proteomics to map druggable proteins that are selectively expressed in KEA

146 echanisms, as well as the discovery of novel druggable proteins within the ubiquitin pathway.

147 tease, (2) a set of previously characterized druggable proteins, and (3) E. coli ketopantoate reducta

148 r beyond traditionally defined categories of druggable proteins.

149 which we have updated, as well as the Human Druggable Proteome, which we have created for the purpos

150 ts and opens new perspectives and identifies druggable receptors from characterization of the ligand

151 ors, have gained increasing consideration as druggable receptors.

152 ecules, which in turn could be exploited as "druggable" receptors in specific types of cancer.

153 ide-binding domain of Epac1 is a potentially druggable region of the protein.

154 utophagy and identify this HDAC isozyme as a druggable regulator of advanced-stage tumor cell surviva

155 reveal conformational switching in KSR as a druggable regulator of oncogenic Ras, and further sugges

156 tors (GPCRs) in brown adipocytes to identify druggable regulators of BAT.

157 Recent findings also indicate that druggable regulators of S-nitrosylation, for example S-n

158 more frequently driven by GAs in the highly druggable RTK/Ras/mitogen-activated protein kinase (MAPK

159 et an intracellular site and reveals a novel druggable site on the HCV protease.

160 ms FTMap and SiteMap and our newly developed Druggable Site Visualizer (DSV) software tool were used

161 ed in flavivirus MTase that can be used as a druggable site.

162 Thus, druggable sites at PPI are not simply sites that are com

163 structural and physicochemical signature of druggable sites at PPI interfaces is sufficiently robust

164 ures of 15 PPI target proteins show that the druggable sites comprise a cluster of binding hot spots,

165 to quantify changes in the accessibility of druggable sites due to conformational changes induced by

166 r the identification and characterization of druggable sites in drug targets.

167 To identify druggable sites in protein-protein interfaces we combine

168 ious structural analyses reveals alternative druggable sites that may be exploited in future drug des

169 lution facilitated the probing of RT for new druggable sites using fragment screening by X-ray crysta

170 rs or if macrocycles will open up novel oral druggable space.

171 les of the zincates and the informers toward druggable-space coverage.

172 rom the polar and cramped (and so not easily druggable) substrate-binding site and can, for the first

173 bilizing p53 cancer mutation Y220C creates a druggable surface crevice.

174 he growth of KRAS-mutant cells, suggesting a druggable synthetic lethal interaction between KRAS and

175 the MDA5/MAVS/IRF7 pathway as a potentially druggable target against CICs.

176 These inhibitors demonstrate that S31N is a druggable target and provide a new starting point to des

177 is work establishes the Galphai-GIV PPI as a druggable target and sets the conceptual and technical f

178 enzymes allows this axis to emerge as a new druggable target and unfolds its promising therapeutic p

179 her validate protein methyltransferases as a druggable target class.

180 cates that extracellular PPIA is a promising druggable target for ALS and support further studies to

181 eam mediator of PERK-driven metastasis and a druggable target for breast cancer therapy.

182 se findings define chromatin as an important druggable target for cancer epigenetic therapy and sugge

183 ir in EOCs, and identify Poltheta as a novel druggable target for cancer therapy.

184 D2 production and could serve as a potential druggable target for inhibiting tumor initiation and met

185 ously unidentified role for PIP5K1alpha as a druggable target for our newly developed compound ISA-20

186 trol of oncogenic signalling and is a highly druggable target for pan-specific receptor clearance in

187 is information introduces IL6 as a potential druggable target for prevention and treatment of K-ras-m

188 tential utility of the endosomal system as a druggable target for signaling.

189 l interrogation spotlights IAV HA as a major druggable target for small-molecule inhibition.

190 Recently CDK9 has emerged as a druggable target for the development of cancer therapeut

191 e results demonstrate that M1 is a promising druggable target for the discovery of a completely new l

192 suggesting that the GABAAR/NFATc4 axis is a druggable target for the therapy of emotional disorders.

193 ously validated T. brucei NMT as a promising druggable target for the treatment of HAT in both stages

194 This pathway may prove a druggable target for the treatment of tumors driven by e

195 They also point to ErbB4/EGFR as a novel, druggable target for therapeutic intervention, especiall

196 ligands of GPR35, and GPR35 may represent a druggable target for treating certain diseases associate

197 kinase PKC-ss (PRKCB) as a disease-specific druggable target for treatment of Ewing sarcoma.

198 y in solid tumors and a generally applicable druggable target for tumor radiosensitization.

199 dings and the demonstration that MUC1-C is a druggable target have provided the experimental basis fo

200 data suggest that PHB1 may serve as a novel, druggable target in CRAF-mediated vemurafenib resistance

201 to identify a kinase that could be used as a druggable target in efforts to develop new treatments fo

202 receptor subtype 5 (mGluR5) may represent a druggable target in identifying new therapeutics for the

203 lin-sensitive tissues and postulate sEH as a druggable target in metabolic diseases.

204 myristoyltransferase (NMT), an essential and druggable target in Trypanosoma cruzi, the causative age

205 g and that DAC3 represents the first readily druggable target linked to VSG ES control in the African

206 hese results suggest that LCK is a potential druggable target protein in KRAS-Dep lung cancers.

207 sults demonstrate that SHP2 phosphatase is a druggable target that cooperates with lipid kinases in i

208 st that pyridoxal kinase is an essential and druggable target that could lead to much needed alternat

209 Wuestefeld et al. now identify a potentially druggable target that enhances hepatocyte proliferation

210 ndocannabinoid signaling can be an appealing druggable target to dampen neuronal activity if pre-exis

211 a proadipogenic factor which may serve as a druggable target to inhibit the turnover and accumulatio

212 ch signaling, implicating AIBP as a possible druggable target to modulate angiogenesis under patholog

213 ceptor signalling might represent a safe and druggable target to restore cognitive functions in old i

214 , these results suggest that PIP4Kgamma is a druggable target whose inhibition enhances productive au

215 While it has long been clear the mPTP is a druggable target, current agents are limited by off-targ

216 the reduction site of cytochrome b is also a druggable target.

217 cept that ENOX1 represents an antiangiogenic druggable target.

218 demonstrating that mutated KRAS is indeed a druggable target.

219 er the parasite's lysyl-tRNA synthetase as a druggable target.

220 rtant role in prostate cancer and could be a druggable target.

221 genic Csn5/Skp2 signaling axis represents a "druggable" target for this novel ERMA.

222 esent the first evidence that gankyrin is a "druggable" target with small molecules.

223 Loss-of-function screens of druggable targetome against cancer stem-like cells.

224 To identify signaling networks and potential druggable targets across tumor microenvironments (TMEs),

225 hus provides a valuable tool for identifying druggable targets and for testing therapeutic strategies

226 ow that 14-3-3 adaptor protein complexes are druggable targets and identify a new class of small mole

227 the discovery of potential mechanism-driven druggable targets and subsequent clinical trials have co

228 Most druggable targets are membrane components, including mem

229 foundation toward identifying and predicting druggable targets based on their network topology.

230 It would be valuable to identify these less-druggable targets before incurring substantial expenditu

231 nhibit cancer-associated genes including non-druggable targets facilitates personalized medicine appr

232 ments novel disease mechanisms and validates druggable targets for diabetic retinopathy.

233 d ECM metalloproteinases may be particularly druggable targets for intervention.

234 o identify both small molecule compounds and druggable targets for MBNL1 upregulation.

235 the melanocyte, with an eye towards finding druggable targets for melanoma prevention.

236 nto carcinogenesis and discerned potentially druggable targets for metastatic colorectal cancer.

237 these findings highlight the JAKs as novel, druggable targets for mitigating the cytokine-driven hyp

238 s, gut hormones offer an expanding family of druggable targets for obesity-diabetes.

239 Furthermore, proteases are druggable targets for the development of new anti-parasi

240 on of toxic materials and could serve as new druggable targets for therapeutic treatment of hypo- or

241 h diet, vitamin synthesis pathways represent druggable targets for therapeutics.

242 impair recovery after trauma and may provide druggable targets for treating victims of acute nervous

243 hanisms in a pervasive disease and validates druggable targets for treatment.

244 Such studies may yield druggable targets for weight loss therapies.

245 However, no druggable targets have been identified to potentiate act

246 lucose homeostasis endorse these hormones as druggable targets in metabolic disorders.

247 d quantitative mass spectrometry to identify druggable targets in metastatic castration-resistant pro

248 H-dependent tumors, identifies two potential druggable targets in the HH pathway, and suggest that si

249 tic ligands, represent the largest family of druggable targets in the human genome.

250 ther, they help define rules for identifying druggable targets in the transcriptome.

251 ally, using molecular profiling, we identify druggable targets in these neurons and show that local i

252 Protein kinases (PKs) are a class of druggable targets in Trypanosoma brucei, the causative a

253 Among these druggable targets is B-cell CLL/lymphoma 2, which when p

254 AS results, pathways related to these known, druggable targets may represent a promising starting poi

255 onditions and consider possible pathways and druggable targets that may be suitable for this objectiv

256 ere is urgent need for the identification of druggable targets that mediate the reinforcing action of

257 cal mechanism without hypoxia provides novel druggable targets to ameliorate and, perhaps, reverse th

258 n of relevant signaling pathways and therein druggable targets to manipulate stem cell behavior effic

259 A large number of potential druggable targets was thus chemically interrogated, but

260 four families, representing the most common druggable targets with an emphasis on understudied prote

261 e in glaucoma treatment has been to identify druggable targets within the conventional aqueous humor

262 nsferases (PRMTs) are envisaged as promising druggable targets, but their role in physiological and p

263 he siRNA library screen failed to reveal any druggable targets, the small-molecule library screen ide

264 Despite substantial efforts to define druggable targets, there are no therapeutic options that

265 To identify novel druggable targets, we carried out an unbiased high-throu

266 physiology of human disease and as important druggable targets.

267 geted instead, thus increasing the number of druggable targets.

268 and may represent a vast pool of potentially druggable targets.

269 flammation, suggesting that bromodomains are druggable targets.

270 of classification, risk-stratification, and druggable targets.

271 has been limited by the absence of discrete druggable targets.

272 RL1 (also called APLNR) and LPHN3, and other druggable targets.

273 hind the disease, and consequently a lack of druggable targets.

274 apid identification of involved pathways and druggable targets.

275 uble minute (MDM)2/p53 complex represent two druggable targets.

276 arked by the realization that they represent druggable targets.

277 The identification of "druggable" targets is an immediate opportunity and chall

278 n interactions (PPIs) are considered poorly "druggable" targets requiring case-by-case validation.

279 tin signatures that can be used to identify "druggable" targets to counter human aging and age-relate

280 three datasets, and (iii) represents novel "druggable" targets.

281 sting of short interfering RNA against 4000 'druggable' targets in an SCLC-derived cell line, NCI-H19

282 sms in a manner that elucidates alternative 'druggable' targets may inform effective long-term treatm

283 significantly broaden the current notion of 'druggable' targets.

284 or advance in validating protein kinases as 'druggable' targets.

285 A target molecule with an appropriate (druggable) tertiary structure is a necessary but not the

286 the pursuit of targets considered to be less druggable that offer potential for development of promis

287 RDEB tissue becomes malignant and offer new druggable therapeutic targets to prevent cSCC onset.

288 of bromodomains has been demonstrated to be druggable through the discovery of potent inhibitors, sp

289 Our findings designate NR0B1 as a druggable transcriptional regulator that supports NRF2-d

290 CtBP2 is thus a druggable transforming oncoprotein critical for the evol

291 ainable by genomic analysis, suggesting that druggable translational and/or post-translational regula

292 Here, we discuss PP2A as a druggable tumour suppressor in view of the possible intr

293 he serine/threonine-specific kinase p38 as a druggable upstream regulator of FOXC2 stability and func

294 allenge by developing a two-armed screen for druggable upstream regulatory kinases in the PAX3/7-FOXO

295 druggable by druglike compounds, may become druggable using compound classes such as macrocycles or

296 Several genetic alterations are intuitively "druggable" with existing agents, for example, kinase-act